Pharmacokinetics and acetylation of sulfa-2-monomethoxine in humans

Biopharmaceutics & Drug Disposition
T B VreeT Miura

Abstract

In humans sulfa-2-monomethoxine (S) is metabolized by N4-acetylation (39.9 +/- 8.0 per cent). After an oral dose, S is eliminated biphasically (t1/2, 5.2 +/- 1.6 h and 13.2 +/- 3.4 h) which is similar in both fast and slow acetylators. The metabolite N4-acetylsulfa-2-monomethoxine (N4) is eliminated monophasically (t1/2, 30.0 +/- 5.7 h). The intrinsic mean residence time (MRT) of N4 is 33.5 +/- 8.8 h. The mean total body clearance of S is 11.6 +/- 2.7 ml min-1, and the Vdss is 12.3 +/- 1.01. The renal clearance of S during the first day was twice as high as on the following days for two of the six volunteers (8 vs 4 ml min-1). The renal clearance of N4 during the first day, for four out of the six volunteers, was twice as high as on the following days (8 vs 4 ml min-1). The protein binding of S is 95 per cent and that of its conjugate N4 98 per cent. Approximately 80 per cent of the oral dose of S is excreted in the urine as parent drug (41.0 +/- 6.2 per cent) and as N4 acetyl conjugate (39.9 +/- 8.0 per cent).

References

Apr 27, 1990·Pharmaceutisch Weekblad. Scientific Edition·T B VreeM Shimoda
Apr 1, 1989·Nihon juigaku zasshi. The Japanese journal of veterinary science·T B VreeK Hoji
Aug 1, 1986·Journal of Pharmaceutical Sciences·P Veng-Pedersen
Oct 1, 1986·Nihon juigaku zasshi. The Japanese journal of veterinary science·Y Takahashi
Jan 1, 1972·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·S R Walker, R T Williams
Oct 1, 1968·The Biochemical Journal·J W BridgesR T Williams
Jun 1, 1970·The Biochemical Journal·R H AdamsonR T Williams
Dec 1, 1970·Nihon juigaku zasshi. The Japanese journal of veterinary science·T OnoderaY Oshima
Dec 1, 1964·Nihon juigaku zasshi. The Japanese journal of veterinary science·S Oishi, T Nakajima
Jun 1, 1984·Nihon juigaku zasshi. The Japanese journal of veterinary science·M ShimodaT Hayama
Aug 1, 1983·Japanese Journal of Pharmacology·M ShimodaT Hayama
Jun 1, 1983·Journal of Veterinary Pharmacology and Therapeutics·T B VreeJ F Nouws
May 1, 1980·Clinical Pharmacokinetics·T B VreeE van der Kleijn

Citations

Jun 8, 2002·Pharmacogenomics·Peter Meisel

Related Concepts

Acetylation
Half-Life
Kidney
Plasma Protein Binding Capacity
Regression Analysis
Sulfamonomethoxine

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